title: A role for rev-erbα ligands in regulation of adipogenesis.
abstract: Rev-erbs are members of the nuclear receptor (NR) transcription factor superfamily and are widely expressed, but are most prevalent in liver, adipose tissue, skeletal muscle and brain. Rev-erbs are key regulators of the circadian rhythm and are expressed in a circadian manner. The discovery that Rev-erbs are ligand-regulated receptors, whose repressive activity is regulated by the endogenous porphyrin ligand, heme, as well as the recent report of the first synthetic Rev-erb ligand, GSK4112/SR6452, suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases. Here, we review the work leading to the discovery that Rev-erbs are indeed ligand-regulated and the role that both natural and synthetic Rev-erb ligands have on adipogenesis.
authors.affiliation: Department of Molecular Therapeutics, The Scripps Research Institute, Jupiter, FL, 33458, USA.
authors.forename: Douglas J
authors.initials: DJ
authors.lastname: Kojetin
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Burris
mesh_terms: D050156:Adipogenesis / Q000235:genetics; D002940:Circadian Rhythm / Q000235:genetics; D015195:Drug Design; D005786:Gene Expression Regulation; D006418:Heme / Q000235:genetics / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D056953:Nuclear Receptor Subfamily 1, Group D, Member 1 / Q000378:metabolism*; D014158:Transcription, Genetic
chemical_list: D008024:Ligands; C064353:NR1D1 protein, human; D056953:Nuclear Receptor Subfamily 1, Group D, Member 1; D006418:Heme